NAPHTHO[1,2-D]THIAZOL-2-AMINE
NAPHTHO[1,2-D]THIAZOL-2-AMINE
![NAPHTHO[1,2-D]THIAZOL-2-AMINE 结构式](https://img.chemicalbook.com/CAS/GIF/40172-65-4.gif)
NAPHTHO[1,2-D]THIAZOL-2-AMINE 性质
| 熔点 | 184-188°C |
|---|---|
| 沸点 | 417.1±28.0 °C(Predicted) |
| 密度 | 1.403±0.06 g/cm3(Predicted) |
| 储存条件 | Keep in dark place,Sealed in dry,2-8°C |
| 溶解度 | 二甲基亚砜：≥30mg/mL |
| 形态 | 固体 |
| 酸度系数(pKa) | 3.50±0.30(Predicted) |
| 颜色 | 米白色 |
| 稳定性 | 供货时可稳定保存 1 年。 DMSO 溶液可在 -20°C 下保存长达 2 个月。 |
| CAS 数据库 | 40172-65-4(CAS DataBase Reference) |
| EPA化学物质信息 | Naphtho[1,2-d]thiazol-2-amine (40172-65-4) |
NAPHTHO[1,2-D]THIAZOL-2-AMINE 用途与合成方法
EC50: 2.9 μM (KCa2.1), 1.9 μM (KCa2.2), 2.9 μM (KCa2.3), 260 nM (KCa3.1)
SKA-31 activates KCa2/3 channels more potently than PK 26124, and is more selective over other Ion channels.
SKA-31 reduces cell viability with IC
50s
of 5.3 μM , 46.9 μM in HCT-116 cells and HCT-8 cells, respectively.
SKA-31 (5.3 μM; 0-96 hours) reduces HCT-116 cells proliferation when added at time zero at 5.3 μM.
SKA-31 triggers apoptosis in HCT-116 cells at 5 μM, and the effect is smaller in HCT-8 cells at 45 μM.
SKA-31 increases the percentage of cells in G0/G1 phase in HCT-116 and HCT-8 cell lines at 5 μM and 45 μM, respectively.
SKA-31 further activates Caspase 3 and reduces Akt phosphorylation induced by CDDP.
SKA-31 has a synergic effect with CDDP also on the inhibition of HCT-116 cell proliferation.
Cell Viability Assay
| Cell Line: | HCT-116 cells, HCT-8 cells |
| Concentration: | |
| Incubation Time: | 24 hours |
| Result: | Reduced cell viability with IC 50s of 5.3 μM , 46.9 μM in HCT-116 and HCT-8, respectively. |
Cell Proliferation Assay
| Cell Line: | HCT-116 cells |
| Concentration: | 5.3 μM |
| Incubation Time: | 0-96 hours |
| Result: | Reduced HCT-116 cells proliferation when added at time zero at IC 50S value. |
Apoptosis Analysis
| Cell Line: | HCT-116 cells, HCT-8 cells |
| Concentration: | 5 μM (HCT-116 cells), 45 μM (HCT-8 cells) |
| Incubation Time: | 24 hours |
| Result: | Triggered apoptosis in HCT-116 cells, and the effect was smaller in HCT-8 cells. |
Cell Cycle Analysis
| Cell Line: | HCT-116 cells, HCT-8 cells |
| Concentration: | 5 μM (HCT-116), 45 μM (HCT-8) |
| Incubation Time: | 24 hours |
| Result: | Increased the percentage of cells in G0/G1 phase in HCT-116 and HCT-8 cell lines. |
Western Blot Analysis
| Cell Line: | HCT-116 cells |
| Concentration: | |
| Incubation Time: | 24 hours |
| Result: | Further activated Caspase 3 and reduced Akt phosphorylation when co-treatment with CDDP in HCT-116 cells. |
SKA-31 is not acutely toxic and has good pharmacokinetic properties.
SKA-31 potentiates native KCa3.1 and KCa2.3 in murine carotid endothelium with EC
50
values of 225 nM and 1.6 μM for KCa3.1 and KCa2.3, respectively.
SKA-31 stimulates KCa3.1 and KCa2.3 in vascular endothelial cells and increases acetylcholine-induced endothelium-derived hyperpolarizing factor (EDHF) -mediated vasodilation.
SKA-31 potentiates EDHF-type vasodilations and lowers blood pressure in mice. Injections of SKA-31 (1-30 mg/kg; i.p.) lower MAP over 24 hours in normotensive wild-type mice but not in KCa3.1(-/-) mice (-/-).
| Animal Model: | 16-25 weeks mice |
| Dosage: | 1 mg/kg, 10 mg/kg, and 30 mg/kg |
| Administration: | Intraperitoneal injection |
| Result: | Lower MAP over 24 hours in normotensive wild-type mice but not in KCa3.1(-/-) mice (-/-). |
NAPHTHO[1,2-D]THIAZOL-2-AMINE 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024-11-08 | HY-111655 | NAPHTHO[1,2-D]THIAZOL-2-AMINE | 40172-65-4 | 5mg | 600 |
| 2024-11-08 | HY-111655 | NAPHTHO[1,2-D]THIAZOL-2-AMINE | 40172-65-4 | 10mM * 1mLin DMSO | 770 |
